A method for loading a therapeutic compound having a cis diol moiety into pre-formed liposomes is described. The method includes adding to a suspension of liposomes (i) the compound to be loaded into the liposomes and (ii) a boronic acid compound, thereby achieving accumulation of the compound within the liposomes.

The invention provides novel solid supports comprising dihydroxyalkyl aminoalkyl and dihydroxyalkylaminobenzyl groups, and methods for making and using them. The supports are particularly useful for immobilizing and derivatizing functionalized boronic acids for use in solid phase synthesis, such as those used in combinatorial chemistries. The compositions and methods of the invention are also useful as scavenger solid supports, e.g., in solution-phase parallel synthesis of small molecule librari...

A reagent having the general formula of General Formula I: ##STR1## wherein group R is an electrophilic or a nucleophilic moiety suitable for reaction of the reagent with a biologically active species; group R.sub.2 is one of H and OH moieties; group R.sub.3 is one of an alkyl and a methylene bearing an electronegative substituent; group Z is one of (CH.sub.2).sub.n and CH.sub.2 O(CH.sub.2 CH.sub.2 O).sub.n.sub..sub.2 , and n is an integer of from 1 to 5, and n.sub.2 is an integer of from 1 to 4...

A process for preparing bisallylboranes of the formula (I) by reacting a diene with sodium borohydride in the presence of an oxidant: ##STR1## in an inert solvent, with the borane generated in situ reacting selectively with the diene to form the bis(allyl)borane of the formula (I) and the substituents R.sup.1 to R.sup.6 having the following meanings: R.sup.1 14 R.sup.6 are H, aryl or substituted or unsubstituted C.sub.1 -C.sub.4 -alkyl or two radicals R may be closed to form a cyclic system. As ...

Disclosed herein is a method for reducing the rate of degradation of proteins in an animal comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.

Disclosed herein is a method for reducing the rate of degradation of proteins in an animal, comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.

A compound of formula (I): ##STR1## in which: R.sub.1 represents hydrogen or acyl, alkyl, benzyl, alkoxycarbonyl, benzyloxycarbonyl, phenoxycarbonyl, 5-[(dimethyl)amino]naphthylsulfonyl, alkoxycarbonylmethyl or carboxymethyl, R.sub.2 represents hydrogen or phenyl, substituted or unsubstituted benzyl, 3-thienylmethyl, 2-pyridylmethyl, diphenylmethyl, fluorenyl, naphthylmethyl, benzocyclobutyl, (dicyclopropylmethyl)methyl, indanyl or (C.sub.3 -C.sub.7 cycloalkyl)methyl, R'.sub.2 represents hydroge...

A compound having the formula: ##STR1## where R.sub.1, R.sub.2, and R.sub.3 are independently hydrogen or C.sub.1-C.sub.4 alkyl; n is 2-4; X is aryl, substituted aryl or C.sub.1-C.sub.6 alkyl; Y is selected from the group consisting of hydrogen, amino acid, dipeptide or tripeptide linked through the C-terminal carboxylic acid, and amine protecting group is presented.

A process for preparing bisallylboranes of the formula (I) by reacting a diene with sodium borohydride in the presence of an oxidant ##STR1## in an inert solvent, with the borane generated in situ reacting selectively with the diene to form the bis(allyl)borane of the formula (I) and the substituents R.sup.1 to R.sup.6 having the following meanings: R.sup.1 -R.sup.6 are H, aryl or substituted or unsubstituted C.sub.1 -C.sub.4 -alkyl or two radicals R may be closed to form a cyclic system. As oxi...

The invention relates to the compounds of formula (I): ##STR1## in which: R.sub.1 denotes hydrogen, acyl, alkoxycarbonyl, benzyloxycarbonyl, phenoxycarbonyl or linear or branched C.sub.1 -C.sub.6 alkyl, substituted or unsubstituted, or R.sub.6 SO.sub.2 -- in which R.sub.6 denotes alkyl, naphthyl, phenyl, benzyl or morpholine, R.sub.2 denotes hydrogen or phenyl, substituted or unsubstituted benzyl, thienylmethyl, (pyridyl)methyl, diphenylmethyl, fluorenyl, naphthylmethyl, benzocyclobutyl, (dicycl...